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Usage

Uses

Used in Pharmaceutical Industry:
4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzoic acid is used as a chemical scaffold for designing new drugs with specific biological activities. Its unique structure allows for the development of compounds with potential anti-cancer, anti-inflammatory, or anti-microbial effects, addressing various medical needs.
Used in Medicinal Research:
In the field of medicinal research, 4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzoic acid serves as a valuable chemical probe. It can be utilized to study biological pathways and mechanisms, contributing to a deeper understanding of disease processes and the discovery of novel therapeutic targets.
Used in Drug Development:
4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzoic acid is employed as a starting point for drug development. Its structural features can be modified to create new compounds with improved pharmacological properties, such as enhanced potency, selectivity, and reduced side effects, ultimately leading to the development of innovative treatments for various diseases.

Upstream product

• 1056634-62-8 ethyl 4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzoate 
• 10389-51-2 1-morpholino-4-nitrobenzene 
• 2524-67-6 4-morpholino-4-yl-phenylamine 
• 100-00-5 4-chlorobenzonitrile 
• 99768-12-4 4-methoxycarbonylphenylboronic acid 
• 1026029-33-3 4-(2-chloropyrimidin-4-yl) methyl benzoate 
• 247234-41-9 1-(4-morpholinophenyl)guanidine 
• 3609-53-8 methyl 4-acetylbenzoate 
• 114431-72-0 (E)-methyl 4-(3-(dimethylamino)acryloyl)benzoate 
• 701215-21-6 methyl 4-[3-(dimethylamino)-1-oxo-2-propen-1-yl]benzoate 
• 499195-60-7 4-(4-carboethoxyphenyl)-2-chloropyrimidine 
• 4334-88-7 p-ethoxycarbonylphenylboronic acid 

Downstream Products

• 1056634-68-4 Momelotinib 
• 1619927-63-7 N-(cyano(d₂-methyl))-4-(2-(4-(morpholinophenyl)amino)pyrimidin-4-yl)benzamide 

Relevant academic research and scientific papers

Synthesis of Imidazoles and Oxazoles via a Palladium-Catalyzed Decarboxylative Addition/Cyclization Reaction Sequence of Aromatic Carboxylic Acids with Functionalized Aliphatic Nitriles

We herein report an efficient approach for the assembly of multiply substituted imidazoles and oxazoles in a single-step manner. These transformations are based on a decarboxylation addition and annulation of readily accessible aromatic carboxylic acids a

Preparation method of JAK inhibitor momelotinib

The invention relates to a preparation method of a JAK inhibitor momelotinib. The preparation method provided by the invention has the advantages of simple preparation route, mild preparation conditions, cheap and easily available raw materials and relatively low synthesis cost.

Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections

Clinically, leukemia patients often suffer from the limited efficacy of chemotherapy and high risks of infection by invasive fungal pathogens. Herein, a novel therapeutic strategy was developed in which a small molecule can simultaneously treat leukemia and invasive fungal infections (IFIs). Novel Janus kinase 2 (JAK2) and histone deacetylase (HDAC) dual inhibitors were identified to possess potent anti-proliferative activity toward hematological cell lines and excellent synergistic effects with fluconazole to treat resistant Candida albicans infections. In particular, compound 20a, a highly active and selective JAK2/HDAC6 dual inhibitor, showed excellent in vivo antitumor efficacy in several acute myeloid leukemia (AML) models and synergized with fluconazole for the treatment of resistant C. albicans infections. This study highlights the therapeutic potential of JAK2/HDAC dual inhibitors in treating AML and IFIs and provides an efficient strategy for multitargeting drug discovery.

New and Practical Synthesis of Momelotinib

New and practical synthetic route of momelotinib, a JAK inhibitor, is described on a decagram scale. A convergent synthetic process is adopted to prepare the methyl 4-(2-((4-morpholinophenyl)amino)pyrimidin-4-yl) benzoate intermediate, by cyclization of 1-(4-morpholinophenyl)guanidine and methyl 4-(3-(dimethylamino)acryloyl)benzoate in high yield and mild conditions. Momelotinib is obtained in 43.2% yield over five steps and 99.1% purity (HPLC).

A method for preparing Momelotinib JAK inhibitors (by machine translation)

The invention relates to a method for the synthesis of inhibitors JAK Momelotinib, chemical medicine, in the field of chemical engineering and technology. Comprises the following steps : (a) the 4 the aniline and morpholine- [...] 50% shan Jingan dissolve

A novel and efficient synthesis of momelotinib

An improved route for the synthesis of momelotinib has been developed. A nucleophilic addition reaction between the starting material, 4-morpholinoaniline, and cyanamide gave the 1-(4-morpholinophenyl)guanidine. Simultaneously, methyl 4-acetylbenzoate was converted into methyl (E)-4-[3-(dimethylamino)acryloyl]benzoate in the presence of N,N-dimethylformamide dimethylacetal. The enaminone intermediate was then condensed at elevated temperature in alcoholic alkali with the 1-(morpholinophenyl)guanidine to form the desired pyrimidine, which was hydrolysed to the corresponding acid. This procedure is simple in operation, without noble metal catalyst and suitable for industrial production. Finally, the desired compound momelotinib was acquired by an amidation reaction.

DEUTERATED PHENYL AMINO PYRIMIDINE COMPOUND AND PHARMACEUTICAL COMPOSITION CONTAINING SAME

The present invention relates to a deuterated phenyl amino pyrimidine compound and pharmaceutical composition containing the same. Specifically provided are a deuterated phenyl amino pyrimidine compound as represented by formula (I), and pharmaceutical composition containing the compound, or polymorph, pharmaceutically acceptable salt, hydrate or solvate thereof. The compound of the present invention can treat and/or prevent JAK kinase-related diseases, such as bone marrow proliferative disease, cancer, immunologic diseases and the like.

PHENYL AMINO PYRIMIDINE COMPOUNDS AND USES THEREOF

The present invention relates to phenyl amino pyrimidine compounds which are inhibitors of protein kinases including JAK kinases. In particular the compounds are selective for JAK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.

4-ARYL-2-AMINO-PYRIMIDINES OR 4-ARYL-2-AMINOALKYL-PYRIMIDINES AS JAK-2 MODULATORS AND METHODS OF USE

This invention relates to certain pyrimidine derivative inhibitors of JAK-2, having Formula (I): wherein D, E, L, Z, R1, R2, R25, and n1 are as defined in the specification, pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof.